Gallic acid isolated from Spirogyra sp. improves cardiovascular disease through a vasorelaxant and antihypertensive effect.

Abstract

In this study, we investigated the vasorelaxant and antihypertensive effects of gallic acid (GA), a polyphenol isolated from the green alga Spirogyra sp., to assess its suitability as a therapeutic for cardiovascular diseases (CVDs). We examined the effect of GA on endothelium-dependent vasorelaxation in human umbilical vein endothelial cells (HUVECs). GA increased nitric oxide (NO) levels by increasing phosphorylation of endothelial nitric oxide synthase (eNOS), and its effect on NO production was attenuated by pretreatment with the eNOS inhibitor N(G)-nitro-L-arginine methyl ester (L-NAME). We also investigated its antihypertensive effect by examining GA-mediated inhibition of angiotensin-I converting enzyme (ACE). GA inhibited ACE with a half-maximal inhibitory concentration (IC50) value of 37.38 ± 0.39 μg/ml. In silico simulations revealed that GA binds to the active site of ACE (PDB: 1O86) with a binding energy of -270.487 kcal/mol. Furthermore, GA clearly reduced blood pressure in spontaneously hypertensive rats (SHR) to an extent comparable to captopril. These results suggest that GA isolated from Spirogyra sp. exerts multiple therapeutic effects and has potential as a CVD treatment.

• Authors: Nalae Kang, Ji-Hyeok Lee, WonWoo Lee, Ju-Young Ko, Eun-A Kim, Jin-Soo Kim, Min-Soo Heu, Gwang Hoon Kim, You-Jin Jeon
• Journal: Environmental toxicology and pharmacology (Environ Toxicol Pharmacol) Vol. 39 Issue 2 Pg. 764-72 (Mar 2015) ISSN: 1872-7077 [Electronic] Netherlands
• PMID: 25727171 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2015 Elsevier B.V. All rights reserved.

Chemical References

• Angiotensin-Converting Enzyme Inhibitors
• Antihypertensive Agents
• Antioxidants
• Vasodilator Agents
• Nitric Oxide
• Gallic Acid
• NOS3 protein, human
• Nitric Oxide Synthase Type III
• Cyclic Nucleotide Phosphodiesterases, Type 3

Topics

• Angiotensin-Converting Enzyme Inhibitors (isolation & purification, pharmacology, therapeutic use)
• Animals
• Antihypertensive Agents (isolation & purification, pharmacology, therapeutic use)
• Antioxidants (isolation & purification, pharmacology, therapeutic use)
• Cardiovascular Diseases (drug therapy, physiopathology)
• Cells, Cultured
• Cyclic Nucleotide Phosphodiesterases, Type 3 (metabolism)
• Gallic Acid (isolation & purification, pharmacology, therapeutic use)
• Human Umbilical Vein Endothelial Cells (drug effects, metabolism)
• Humans
• Male
• Nitric Oxide (metabolism)
• Nitric Oxide Synthase Type III (metabolism)
• Rats
• Rats, Inbred SHR
• Spirogyra (chemistry)
• Vasodilator Agents (isolation & purification, pharmacology, therapeutic use)